JP4495456B2 - 新規の抗炎症性アンドロスタン誘導体 - Google Patents
新規の抗炎症性アンドロスタン誘導体 Download PDFInfo
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- JP4495456B2 JP4495456B2 JP2003538181A JP2003538181A JP4495456B2 JP 4495456 B2 JP4495456 B2 JP 4495456B2 JP 2003538181 A JP2003538181 A JP 2003538181A JP 2003538181 A JP2003538181 A JP 2003538181A JP 4495456 B2 JP4495456 B2 JP 4495456B2
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- compound
- methyl
- oxy
- acid
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- KHPXUQMNIQBQEV-UHFFFAOYSA-N oxaloacetic acid Chemical compound OC(=O)CC(=O)C(O)=O KHPXUQMNIQBQEV-UHFFFAOYSA-N 0.000 description 1
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- 229960000797 oxitropium Drugs 0.000 description 1
- MUMZUERVLWJKNR-UHFFFAOYSA-N oxoplatinum Chemical compound [Pt]=O MUMZUERVLWJKNR-UHFFFAOYSA-N 0.000 description 1
- AFDXODALSZRGIH-UHFFFAOYSA-N p-coumaric acid methyl ether Natural products COC1=CC=C(C=CC(O)=O)C=C1 AFDXODALSZRGIH-UHFFFAOYSA-N 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
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- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 229920000053 polysorbate 80 Polymers 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
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- 102000004169 proteins and genes Human genes 0.000 description 1
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- 125000003373 pyrazinyl group Chemical group 0.000 description 1
- 125000002098 pyridazinyl group Chemical group 0.000 description 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
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- 125000003808 silyl group Chemical group [H][Si]([H])([H])[*] 0.000 description 1
- 208000017520 skin disease Diseases 0.000 description 1
- KKCBUQHMOMHUOY-UHFFFAOYSA-N sodium oxide Chemical compound [O-2].[Na+].[Na+] KKCBUQHMOMHUOY-UHFFFAOYSA-N 0.000 description 1
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- XCAQIUOFDMREBA-UHFFFAOYSA-N tert-butyl n-[(2-methylpropan-2-yl)oxycarbonyl]carbamate Chemical compound CC(C)(C)OC(=O)NC(=O)OC(C)(C)C XCAQIUOFDMREBA-UHFFFAOYSA-N 0.000 description 1
- HMLHNVLIQQGYRO-UHFFFAOYSA-N tert-butyl n-[2-(2,2-dimethyl-4h-1,3-benzodioxin-6-yl)-2-oxoethyl]-n-[(2-methylpropan-2-yl)oxycarbonyl]carbamate Chemical compound O1C(C)(C)OCC2=CC(C(=O)CN(C(=O)OC(C)(C)C)C(=O)OC(C)(C)C)=CC=C21 HMLHNVLIQQGYRO-UHFFFAOYSA-N 0.000 description 1
- YIIVONGCNAQATO-UHFFFAOYSA-N tert-butyl n-[2-(2,2-dimethyl-4h-1,3-benzodioxin-6-yl)-2-oxoethyl]carbamate Chemical compound O1C(C)(C)OCC2=CC(C(=O)CNC(=O)OC(C)(C)C)=CC=C21 YIIVONGCNAQATO-UHFFFAOYSA-N 0.000 description 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
- C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
- A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0125259.2A GB0125259D0 (en) | 2001-10-20 | 2001-10-20 | Novel compounds |
| PCT/EP2002/011634 WO2003035668A2 (en) | 2001-10-20 | 2002-10-17 | Novel anti-inflammatory androstane derivatives -17-carboxy-lactone substituted steroids with an aryl-carboxylic ester in position 17.alpha |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005509642A JP2005509642A (ja) | 2005-04-14 |
| JP2005509642A5 JP2005509642A5 (enrdf_load_stackoverflow) | 2006-01-05 |
| JP4495456B2 true JP4495456B2 (ja) | 2010-07-07 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003538181A Expired - Lifetime JP4495456B2 (ja) | 2001-10-20 | 2002-10-17 | 新規の抗炎症性アンドロスタン誘導体 |
Country Status (9)
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| US6777399B2 (en) | 2000-08-05 | 2004-08-17 | Smithkline Beecham Corporation | Anti-inflammatory androstane derivative compositions |
| US6858593B2 (en) | 2000-08-05 | 2005-02-22 | Smithkline Beecham Corporation | Anti-inflammatory androstane derivative compositions |
| US6858596B2 (en) | 2000-08-05 | 2005-02-22 | Smithkline Beecham Corporation | Formulation containing anti-inflammatory androstane derivative |
| GB0019172D0 (en) | 2000-08-05 | 2000-09-27 | Glaxo Group Ltd | Novel compounds |
| CA2634715A1 (en) | 2000-08-05 | 2002-02-14 | Glaxo Group Limited | 6.alpha.,9.alpha.-difluoro-17.alpha.-[(2-furanylcarboxyl)oxy}-11.beta.-hydroxy-16.alpha-methyl-3-oxo-androsta-1,4-diene-17.beta.carbothioic acids-fluoromethyl ester as an anti-inflammatory agent |
| UA77656C2 (en) | 2001-04-07 | 2007-01-15 | Glaxo Group Ltd | S-fluoromethyl ester of 6-alpha, 9-alpha-difluoro-17-alpha-[(2-furanylcarbonyl)oxy]-11-beta-hydroxy-16- alpha-methyl-3-oxoandrosta-1,4-dien-17-beta-carbothioacid as anti-inflammatory agent |
| CA2445839A1 (en) | 2001-04-30 | 2002-11-07 | Glaxo Group Limited | Anti-inflammatory 17.beta.-carbothioate ester derivatives of androstane with a cyclic ester group in position 17.alpha |
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| AR044519A1 (es) | 2003-05-02 | 2005-09-14 | Novartis Ag | Derivados de piridin-tiazol amina y de pirimidin-tiazol amina |
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| AU2006277769B2 (en) | 2005-08-08 | 2011-06-02 | Pulmagen Therapeutics (Synergy) Limited | Bicyclo[2.2.1]hept-7-ylamine derivatives and their uses |
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| TWI374147B (en) * | 2006-01-27 | 2012-10-11 | Sun Pharma Advance Res Company Ltd | Novel 11β-hydroxyandrosta-4-ene-3-ones |
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| ATE549337T1 (de) | 2006-04-21 | 2012-03-15 | Novartis Ag | Purinderivate zur verwendung als adenosin-a2a- rezeptoragonisten |
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| PL2104535T3 (pl) | 2007-01-10 | 2011-05-31 | Irm Llc | Związki i kompozycje jako inhibitory proteazy aktywujące kanały |
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| MX2010006421A (es) | 2007-12-10 | 2010-06-25 | Novartis Ag | Compuestos organicos. |
| CN102112130A (zh) | 2008-06-10 | 2011-06-29 | 诺瓦提斯公司 | 作为上皮钠通道阻滞剂的吡嗪衍生物 |
| EA019441B1 (ru) | 2008-12-30 | 2014-03-31 | Палмаджен Терепьютикс (Инфлеммейшн) Лимитед | Сульфонамиды, предназначенные для лечения респираторных нарушений |
| JP2012516345A (ja) | 2009-01-29 | 2012-07-19 | ノバルティス アーゲー | 星細胞腫治療用置換ベンゾイミダゾール |
| CA2764830A1 (en) | 2009-06-16 | 2010-12-23 | Schering Corporation | Novel [3,2-c] heteroaryl steroids as glucocorticoid receptor agonists, compositions and uses thereof |
| US8389526B2 (en) | 2009-08-07 | 2013-03-05 | Novartis Ag | 3-heteroarylmethyl-imidazo[1,2-b]pyridazin-6-yl derivatives |
| KR20120089643A (ko) | 2009-08-12 | 2012-08-13 | 노파르티스 아게 | 헤테로시클릭 히드라존 화합물, 및 암 및 염증을 치료하기 위한 그의 용도 |
| IN2012DN01961A (enrdf_load_stackoverflow) | 2009-08-17 | 2015-08-21 | Intellikine Llc | |
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| MX2012004792A (es) | 2009-10-22 | 2013-02-01 | Vertex Pharma | Composiciones para el tratamiento de fibrosis quistica y otras enfermedades cronicas. |
| US8247436B2 (en) | 2010-03-19 | 2012-08-21 | Novartis Ag | Pyridine and pyrazine derivative for the treatment of CF |
| UY33597A (es) | 2010-09-09 | 2012-04-30 | Irm Llc | Compuestos y composiciones como inhibidores de la trk |
| WO2012034095A1 (en) | 2010-09-09 | 2012-03-15 | Irm Llc | Compounds and compositions as trk inhibitors |
| US8372845B2 (en) | 2010-09-17 | 2013-02-12 | Novartis Ag | Pyrazine derivatives as enac blockers |
| EP2673277A1 (en) | 2011-02-10 | 2013-12-18 | Novartis AG | [1, 2, 4]triazolo [4, 3 -b]pyridazine compounds as inhibitors of the c-met tyrosine kinase |
| EP2678016B1 (en) | 2011-02-23 | 2016-08-10 | Intellikine, LLC | Heterocyclic compounds and uses thereof |
| PH12013501758A1 (en) | 2011-02-25 | 2013-10-14 | Irm Llc | Pyrazolo [1,5-a] pyridines as trk inhibitors |
| UY34305A (es) | 2011-09-01 | 2013-04-30 | Novartis Ag | Derivados de heterociclos bicíclicos para el tratamiento de la hipertensión arterial pulmonar |
| CA2848809A1 (en) | 2011-09-15 | 2013-03-21 | Novartis Ag | 6-substituted 3-(quinolin-6-ylthio)-[1,2,4]triazolo[4,3-a]pyradines as c-met tyrosine kinase |
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| WO2013038386A1 (en) | 2011-09-16 | 2013-03-21 | Novartis Ag | Heterocyclic compounds for the treatment of cystic fibrosis |
| HK1203378A1 (en) | 2011-11-23 | 2015-10-30 | Intellikine, Llc | Enhanced treatment regimens using mtor inhibitors |
| US8809340B2 (en) | 2012-03-19 | 2014-08-19 | Novartis Ag | Crystalline form |
| ES2894830T3 (es) | 2012-04-03 | 2022-02-16 | Novartis Ag | Productos combinados con inhibidores de tirosina·cinasa y su uso |
| US9073921B2 (en) | 2013-03-01 | 2015-07-07 | Novartis Ag | Salt forms of bicyclic heterocyclic derivatives |
| WO2014151147A1 (en) | 2013-03-15 | 2014-09-25 | Intellikine, Llc | Combination of kinase inhibitors and uses thereof |
| EP3007697B1 (en) | 2013-06-14 | 2020-09-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Rac1 inhibitors for inducing bronchodilation |
| WO2015084804A1 (en) | 2013-12-03 | 2015-06-11 | Novartis Ag | Combination of mdm2 inhibitor and braf inhibitor and their use |
| EA032075B1 (ru) | 2014-04-24 | 2019-04-30 | Новартис Аг | Производные аминопиразина в качестве ингибиторов фосфатидилинозитол-3-киназы |
| US10112926B2 (en) | 2014-04-24 | 2018-10-30 | Novartis Ag | Amino pyridine derivatives as phosphatidylinositol 3-kinase inhibitors |
| CA2945257A1 (en) | 2014-04-24 | 2015-10-29 | Novartis Ag | Pyrazine derivatives as phosphatidylinositol 3-kinase inhibitors |
| WO2016011658A1 (en) | 2014-07-25 | 2016-01-28 | Novartis Ag | Combination therapy |
| US10195208B2 (en) | 2014-07-31 | 2019-02-05 | Novartis Ag | Combination therapy |
| CA3139634A1 (en) | 2019-06-10 | 2020-12-17 | Novartis Ag | Pyridine and pyrazine derivative for the treatment of cf, copd, and bronchiectasis |
| PH12022550468A1 (en) | 2019-08-28 | 2023-03-06 | Novartis Ag | Substituted 1,3-phenyl heteroaryl derivatives and their use in the treatment of disease |
| TW202140550A (zh) | 2020-01-29 | 2021-11-01 | 瑞士商諾華公司 | 使用抗ｔｓｌｐ抗體治療炎性或阻塞性氣道疾病之方法 |
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| US3828080A (en) * | 1972-01-20 | 1974-08-06 | Glaxo Lab Ltd | Androstane-17beta-carboxylic acids and processes for the preparation thereof |
| GB1438940A (en) * | 1972-07-19 | 1976-06-09 | Glaxo Lab Ltd | 17beta-haloalkoxycarbonyl-17alpha-oxysteroids |
| ATE8790T1 (de) * | 1981-02-02 | 1984-08-15 | Schering Corporation | Aromatische heterocyclische steroidester, verfahren zu ihrer herstellung und pharmazeutische zusammensetzungen, die sie enthalten. |
| US6197761B1 (en) * | 1995-12-29 | 2001-03-06 | Glaxo Wellcome Inc. | 17β-2-oxo-tetrahydrofuranyl)-carbothioic acid ester, -carboxylic acid ester and -carboxylic acid amide androstane derivatives |
| GB0015876D0 (en) * | 2000-06-28 | 2000-08-23 | Novartis Ag | Organic compounds |
| US6777400B2 (en) * | 2000-08-05 | 2004-08-17 | Smithkline Beecham Corporation | Anti-inflammatory androstane derivative compositions |
| US6858596B2 (en) * | 2000-08-05 | 2005-02-22 | Smithkline Beecham Corporation | Formulation containing anti-inflammatory androstane derivative |
| US6858593B2 (en) * | 2000-08-05 | 2005-02-22 | Smithkline Beecham Corporation | Anti-inflammatory androstane derivative compositions |
| US6750210B2 (en) * | 2000-08-05 | 2004-06-15 | Smithkline Beecham Corporation | Formulation containing novel anti-inflammatory androstane derivative |
| CA2634715A1 (en) * | 2000-08-05 | 2002-02-14 | Glaxo Group Limited | 6.alpha.,9.alpha.-difluoro-17.alpha.-[(2-furanylcarboxyl)oxy}-11.beta.-hydroxy-16.alpha-methyl-3-oxo-androsta-1,4-diene-17.beta.carbothioic acids-fluoromethyl ester as an anti-inflammatory agent |
| US6759398B2 (en) * | 2000-08-05 | 2004-07-06 | Smithkline Beecham Corporation | Anti-inflammatory androstane derivative |
| GB0019172D0 (en) * | 2000-08-05 | 2000-09-27 | Glaxo Group Ltd | Novel compounds |
| US6777399B2 (en) * | 2000-08-05 | 2004-08-17 | Smithkline Beecham Corporation | Anti-inflammatory androstane derivative compositions |
| US6787532B2 (en) * | 2000-08-05 | 2004-09-07 | Smithkline Beecham Corporation | Formulation containing anti-inflammatory androstane derivatives |
| GB0103630D0 (en) * | 2001-02-14 | 2001-03-28 | Glaxo Group Ltd | Chemical compounds |
| UA77656C2 (en) * | 2001-04-07 | 2007-01-15 | Glaxo Group Ltd | S-fluoromethyl ester of 6-alpha, 9-alpha-difluoro-17-alpha-[(2-furanylcarbonyl)oxy]-11-beta-hydroxy-16- alpha-methyl-3-oxoandrosta-1,4-dien-17-beta-carbothioacid as anti-inflammatory agent |
| AU2003244451A1 (en) * | 2002-02-04 | 2003-09-02 | Glaxo Group Limited | Amorphous fluticasone 2-furoate, pharmaceutical compositions thereof and its conversion to the crystalline unsolvated form |
| US20050175545A1 (en) * | 2002-02-04 | 2005-08-11 | Keith Biggadike | Formulation for inhalation comprising a glucocorticoid and a beta 2-adrenoreceptor agonist |
| GB0316290D0 (en) * | 2003-07-11 | 2003-08-13 | Glaxo Group Ltd | Novel compounds |
-
2001
- 2001-10-20 GB GBGB0125259.2A patent/GB0125259D0/en not_active Ceased
-
2002
- 2002-10-17 JP JP2003538181A patent/JP4495456B2/ja not_active Expired - Lifetime
- 2002-10-17 WO PCT/EP2002/011634 patent/WO2003035668A2/en active IP Right Grant
- 2002-10-17 EP EP02785235A patent/EP1444248B1/en not_active Expired - Lifetime
- 2002-10-17 ES ES02785235T patent/ES2304457T3/es not_active Expired - Lifetime
- 2002-10-17 DE DE60226334T patent/DE60226334T2/de not_active Expired - Lifetime
- 2002-10-17 AU AU2002350561A patent/AU2002350561A1/en not_active Abandoned
- 2002-10-17 US US10/492,813 patent/US7405206B2/en not_active Expired - Lifetime
- 2002-10-17 AT AT02785235T patent/ATE393771T1/de not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| DE60226334T2 (de) | 2009-06-04 |
| US20050054622A1 (en) | 2005-03-10 |
| WO2003035668A2 (en) | 2003-05-01 |
| EP1444248B1 (en) | 2008-04-30 |
| AU2002350561A1 (en) | 2003-05-06 |
| EP1444248A2 (en) | 2004-08-11 |
| ATE393771T1 (de) | 2008-05-15 |
| WO2003035668A3 (en) | 2003-07-31 |
| ES2304457T3 (es) | 2008-10-16 |
| US7405206B2 (en) | 2008-07-29 |
| GB0125259D0 (en) | 2001-12-12 |
| JP2005509642A (ja) | 2005-04-14 |
| DE60226334D1 (de) | 2008-06-12 |
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